Author/Authors :
Takeshi Masuda، نويسنده , , Satoshi Shibuya، نويسنده , , Masami Arai، نويسنده , , Shuku Yoshida، نويسنده , , Takanori Tomozawa، نويسنده , , Akiko Ohno، نويسنده , , Makoto Yamashita، نويسنده , , Takeshi Honda، نويسنده ,
Abstract :
We synthesized bicyclic ether sialidase inhibitors such as tetrahydro-furan-2-yl, tetrahydro-pyran-2-yl, and oxepan-2-yl derivatives related to zanamivir. These compounds substituted by diol at the C-3′ and C-4′ positions resulted in the retention of low nanomolar inhibitory activities against not only influenza A virus sialidase but also influenza A virus in cell culture. Compound 11a in particular showed comparable efficacy in vivo relative to that of oseltamivir phosphate.
